Pharmaceutical compositions comprising safinamide

Abstract

The present invention relates to pharmaceutical compositions comprising safinamide and, more particularly, to taste-masked particles comprising said active ingredient or pharmaceutically acceptable salts thereof, oral dosage forms that include said particles and a process for preparing them.

The invention claimed is: 
     
       1. A plurality of particles, wherein each particle of the plurality of particles comprises:
 a. a core comprising safinamide or a pharmaceutically acceptable salt thereof; and 
 b. a taste-masking polymer composition which forms a coating on said core; 
 wherein said core comprises an inert particle layered with said safinamide or a pharmaceutically acceptable salt thereof in the presence of a binder. 
 
     
     
       2. A plurality of particles according to  claim 1  wherein each particle of the plurality of particles has a particle size of not more than 500 μm. 
     
     
       3. A plurality of particles according to  claim 1  wherein said core comprises safinamide methanesulfonate. 
     
     
       4. A plurality of particles according to  claim 1  wherein said binder is selected among povidone (PVP), polyethylene glycol (PEG), pregelatinized starch, hydroxypropyl methylcellulose (HPMC), microcrystalline cellulose and a mixture thereof. 
     
     
       5. A plurality of particles according to  claim 1  wherein said inert particle is a particle of microcrystalline cellulose. 
     
     
       6. A plurality of particles according to  claim 1  wherein said taste-masking polymer composition is present in an amount comprised between 10 and 70 wt. %. 
     
     
       7. A plurality of particles according to  claim 6  wherein said taste-masking polymer composition is present in an amount comprised between 20 and 40 wt. %. 
     
     
       8. A plurality of particles according to  claim 1  wherein said taste-masking polymer composition comprises a mixture of water-soluble cellulose-based polymers and water-insoluble cellulose-based polymers. 
     
     
       9. A plurality of particles according to  claim 1  wherein said taste-masking polymer composition comprises a plasticizer. 
     
     
       10. A plurality of particles according to  claim 9  wherein said plasticizer is present in an amount of not less than 2 wt. % based on the weight of each particle. 
     
     
       11. A plurality of particles according to  claim 1 , wherein said taste masking polymer composition comprises basic polymethacrylate butylate, ethylcellulose, ethylcellulose mixed with hydroxypropylmethylcellulose, or ethylcellulose mixed with basic polymethacrylate butylate. 
     
     
       12. A plurality of particles according to  claim 8 , wherein said mixture of said water-soluble cellulose-based polymers and said water-insoluble cellulose-based polymers comprises ethylcellulose mixed hydroxypropylcellulose. 
     
     
       13. An orally disintegrating tablet comprising a plurality of particles according to  claim 1 . 
     
     
       14. An orally disintegrating tablet according to  claim 13  comprising:
 a) 20-70 wt. % of the plurality of particles; 
 b) 20-40 wt. % of a diluent; 
 c) 2-20 wt. % of a binder; 
 d) 7-16 wt. % of a disintegrant; 
 e) 1-4 wt. % of a lubricant, 
 wherein the combined concentration a)-e) is 100 wt. %. 
 
     
     
       15. A process for preparing a plurality of particles according to  claim 1  which comprises:
 a. layering safinamide or a pharmaceutical acceptable salt thereof in the presence of a binder on an inert particle to form a core; and 
 b. coating said core with a taste-masking polymer composition. 
 
     
     
       16. A process according to  claim 15 , wherein in step a. said safinamide or said pharmaceutical acceptable salt thereof is dissolved or dispersed in an aqueous vehicle in the presence of said binder. 
     
     
       17. A method of preparing an oral dosage form comprising mixing a plurality of particles according to  claim 1  with pharmaceutically acceptable excipients.